Fragment-based discovery and optimization of BACE1 inhibitors
Autor: | Myron A. Smith, Marion Biniszkiewicz, David James Hallett, John Barker, Jenny R. Dod, James Madden, Joachim Kraemer, Robert Godemann, Jane Dannow Dyekjaer, Thomas Hesterkamp |
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Rok vydání: | 2010 |
Předmět: |
Models
Molecular 2-aminobenzimidazole Drug discovery Stereochemistry Chemistry Memapsin-2 Organic Chemistry Clinical Biochemistry Pharmaceutical Science Computational biology Biochemistry Structure-Activity Relationship Fragment (logic) Drug Discovery Molecular Medicine Aspartic Acid Endopeptidases Humans Protease Inhibitors Amyloid Precursor Protein Secretases Aspartic Endopeptidases Molecular Biology |
Zdroj: | Bioorganicmedicinal chemistry letters. 20(17) |
ISSN: | 1464-3405 |
Popis: | A novel series of 2-aminobenzimidazole inhibitors of BACE1 has been discovered using fragment-based drug discovery (FBDD) techniques. The rapid optimization of these inhibitors using structure-guided medicinal chemistry is discussed. |
Databáze: | OpenAIRE |
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